ChemicalBook--->CAS DataBase List--->864374-00-5

864374-00-5

864374-00-5 Structure

864374-00-5 Structure
IdentificationBack Directory
[Name]

TP0427736
[CAS]

864374-00-5
[Synonyms]

TP0427736
TP0427736 HCl
[Molecular Formula]

C14H10N4S2
[MDL Number]

MFCD32644807
[MOL File]

864374-00-5.mol
[Molecular Weight]

298.39
Chemical PropertiesBack Directory
[Boiling point ]

634.7±65.0 °C(Predicted)
[density ]

1.439±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 67 mg/mL (200.09 mM);Ethanol: Insoluble
[pka]

9.70±0.10(Predicted)
[Water Solubility ]

Water: Insoluble
Hazard InformationBack Directory
[Uses]

TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells[1].
[Biological Activity]

TP0427736 is a potent ALK5 kinase inhibitor with IC50 of 2.72 nM and IC50 of 836 nM for ALK3. It also inhibits TGF-β1-induced phosphorylation of Smad2/3 in A549 cells with IC50 of 8.68 nM.
[in vitro]

TP0427736 can inhibit Smad2/3 phosphorylation in a concentration-dependent manner with IC50 of 8.68 nM. In outer root sheath cells, it rescued the inhibition of cell proliferation by TGF-β1 and TGF-β2.

[in vivo]

TP0427736 reduces hair follicle length shortening during the transition from anagen to catagen.

[target]

TargetValue
ALK5
(Cell-free assay)
2.72 nM
[storage]

Store at -20°C
[References]

[1] Naruse T, et al. Novel ALK5 inhibitor TP0427736 reduces TGF-βinduced growth inhibition in human outer root sheath cells and elongates anagen phase in mouse hair follicles. Pharmacol Rep. 2017 Jun;69(3):485-491. DOI:10.1016/j.pharep.2017.01.024
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